mifepristone, Mifeprex

Omudhome Ogbru, PharmD

Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

Jay W. Marks, MD

Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

GENERIC NAME: mifepristone

BRAND NAME: Mifeprex, Korlym

DRUG CLASS AND MECHANISM: Mifepristone is a synthetic steroid with
antiprogesterone and antiglucocorticoid effects. It is used for terminating
pregnancy and treating people with Cushing syndrome. Progesterone is a female
hormone and the principal progestational hormone. Progesterone prepares the
uterus (the womb) to receive and sustain the fertilized egg andis an important
hormone for sustaining pregnancy. Mifepristone terminates early pregnancy by
blocking the activity of progesterone at progesterone receptors. It also
stimulates contraction of the uterus. Early pregnancy is considered to be = 49
days (7weeks) since the last menstrual period began. Mifepristone must be used
in combination with misoprostol for the purpose of termination of pregnancy. The
FDA approved this combination treatment in September 2000.

Cortisol is a metabolite (break down product) of the hormone cortisone.
Cortisol is an essential factor in many processes including the proper
metabolism of starches, and it is the major natural glucocorticoid in humans.
People with Cushing syndrome produce too much cortisol, and, among many other
effects, develop high glucose (sugar) levels in the blood. Mifepristone reduces
blood glucose levels in people with Cushing syndrome by blocking the activity of
cortisol.

Day 1: Three 200 mg tablets (600
mg) of mifepristone are taken as a single dose.

Day 3: 400 mcg of misoprostol is
given orally unless abortion has been confirmed.

Day 14: No medication
administered. Patient returns for a post-treatment examination to confirm that a
complete termination of pregnancy has occurred.

The dose for treating Cushing syndrome is 300 mg daily initially. The dose
may be increased to 1200 mg daily.

DRUG INTERACTIONS:Ketoconazole, itraconazole (Sporanox), erythromycin, and
grapefruit juice may increase blood levels of mifepristone by inhibiting the
enzyme responsible for metabolizing (breaking down) mifepristone. Rifampin,
dexamethasone, St. John's Wort,phenytoin, phenobarbital, and carbamazepine may
decrease blood levels of mifepristone by increasing the activity of the enzyme
responsible for metabolizing mifepristone and decrease the effectiveness of
mifepristone. Mifepristone may inhibit liver enzymes which are responsible for
the metabolism of various drugs, resulting in increased blood levels of these
drugs.

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mifepristone, Mifeprex

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